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2-Chloro-N-pyrimidin-5-yl-acetamide → (R)-3-(1-Phenyl-cycloheptanecarbonyloxy)-1-(pyrimidin-5-ylcarbamoylmethyl)-1-azonia-bicyclo[2.2.2]octane chloride
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-Chloro-N-pyrimidin-5-yl-acetamide | HCID 20208139 | — |
| 反応物 | 1-Phenyl-cycloheptanecarboxylic acid (R)-(1-aza-bicyclo[2.2.2]oct-3-yl)ester | HCID 59179619 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | (R)-3-(1-Phenyl-cycloheptanecarbonyloxy)-1-(pyrimidin-5-ylcarbamoylmethyl)-1-azonia-bicyclo[2.2.2]octane chloride | HCID 86655300 | 86.2% |
反応手順
1-Phenyl-cycloheptanecarboxylic acid (R)-(1-aza-bicyclo[2.2.2]oct-3-yl)ester (Example 14e) (115 mg) in acetonitrile (2 mL) was treated with 2-chloro-N-pyrimidin-5-yl-acetamide (Example 52a) (66 mg) to give a dark brown solution that was stirred at room temperature overnight. The resulting solid was filtered off, washed with cold acetonitrile (2 mL) and pentane (3 mL) and dried under vacuum at 45° C. to give the title compound as a tan solid (151 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08329729B2 |
| 出典データセット | uspto-grants-2012_12 |
| ORD ID | ord-76e3315c2be64725aac36c468c1f53b6 |
| 出典メモ | uspto-grants-2012_12 |